A racemate prodrug of leteprinim and methods of making and using the same

By constructing a rasimod prodrug and using a riboflavin derivative to cleave the TK bond under ultrasound activation to release R848, the problems of rasimod's lack of tumor selectivity and systemic toxicity were solved, achieving selective activation and precision treatment at the tumor site.

CN119185313BActive Publication Date: 2026-05-29CHANGCHUN INSTITUTE OF APPLIED CHEMISTRY CHINESE ACADEMY OF SCIENCES
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Patent Information

Application Number
CN202411386054.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-09-30
Publication Date
2026-05-29
Estimated Expiration
2044-09-30

AI Technical Summary

Technical Problem

Resimod (R848) lacks tumor selectivity and causes severe systemic toxicity after administration, thus failing to achieve further clinical application.

Method used

Design a rasimodil prodrug comprising a riboflavin derivative bonded to a carrier R848-TK and mPEG-b-PHEA, construct an ultrasound-activated rasimodil prodrug, and release the active drug R848 by generating 1O2 to cleave the TK bond under ultrasound conditions through the riboflavin derivative.

Benefits of technology

It achieves selective activation of drugs at the tumor site, reduces drug toxicity, enables spatiotemporally controllable precision treatment, and significantly inhibits tumor growth.

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Abstract

The application provides a resiquimod prodrug and a preparation method and application thereof. The resiquimot prodrug comprises a carrier and a riboflavin derivative loaded on the carrier. The carrier is obtained by bonding R848-TK and mPEG-PHEA. b The application uses R848 NPs as a carrier to physically load a liposoluble riboflavin derivative, and is used for constructing an ultrasound-activated resiquimot prodrug. The riboflavin derivative is a liposoluble substance, can be activated under ultrasound conditions, and then generates 1 O2, is used for cutting the TK bond, thereby releasing the active drug R848. The application can effectively enhance the tumor selectivity of the drug and realize a time-space controllable precise treatment by preparing a more specific ultrasound-activated resiquimot prodrug.
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